Characteristics of polymers enabling nano-comminution of water-insoluble drugs

Lee, J.; Choi, Ji-Yeun; Park, Chul Ho

doi:10.1016/j.ijpharm.2007.12.032

Cited by 127 publications

(78 citation statements)

References 26 publications

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“…The mean calibration curve of IBU (regression equation: y = 0.043x + 0.0013) in the dissolution medium over a concentration range of 4-20 µg/mL at 222 nm (λ max ) was found to be linear (n = 6) with a correlation coefficient of r 2 = 0.9993. The in vitro release profiles were evaluated, on the basis of percentage of drug dissolved at 15 min and 60 min (DP 15 and DP 60 ). The reported values [ Table 3] were obtained by calculating the arithmetic mean of three measurements.…”

Section: In Vitro Dissolution Of Ibu From Lyophilized Ibu: Pvp-k30nanmentioning

confidence: 99%

“…Although nano-comminution has advantages, such as cost effectiveness and easy scale-up, the processing is significantly sensitive to the selection of a polymeric stabilizer. [15] The instability of the finely divided particles and their tendency to agglomerate is due to increase the effective surface of the drug particles, which is associated with a proportional vast increase of the surface energy. [16] Among the preparation methods of nanoparticles, nano-comminution has conveniently been utilized to prepare solid nanoparticles due to simplicity and cost-effectiveness.…”

Section: Introductionmentioning

confidence: 99%

“…Many authors concluded that the preparation of drug nanoparticles via nano-comminution requires a series of trial and error experiments because there is a lack of systematic knowledge of the process. [15] High-pressure homogenization technology was found as a simple, effective, well-established technique and can be scaled up to an industrial level. [21] This method was found previously to be an efficient technique to prepare stable nanosuspensions of several drugs such as diclofenac, [22] paclitaxel, [23] budesonide, [24] clofazimine, [25] nifidepine, [26] bupravaquone, [27] amphotericin B, [28] and spironolactone.…”

Section: Introductionmentioning

confidence: 99%

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Introduction: Ibuprofen (IBU), a well-known drug with dissolution rate-limited bioavailability was formulated as nanoparticles and nanosuspensions by ultra-homogenization technique, employing a series of hydrophilic polymers/surfactants. Materials and Methods: Various nanosuspensions were prepared using different hydrophilic polymers, freeze-dried into nano-particles and evaluated for relevant physicochemical characteristics. Based on the in vitro dissolution and particle size, the optimized drug: Polymer ratio was re-formulated into nanosuspensions using Tween-80 to study any further reduction in particle size and enhancement in dissolution as compared with marketed suspensions. Results and Discussion: All the suspensions prepared with the different drugs: Polymer ratio (1:1, 1:2 and 1:3) showed a significant decrease in particle size with increase in the number of homogenization cycles and pressure. Polyvinyl pyrrolidone K30 (PVP-K30) served as the best polymer to enhance the aqueous solubility of IBU, based on stability constant (K) and Gibbsfree energy (ΔG o ) values. IBU: PVP-K30 (1:2 w/w) nanosuspensions gave the least particle size (527 ± 31.04 nm) with a narrow polydispersibility index and high negative zeta potential value. Nanoparticles produced by freeze drying the nano-suspension were amorphous in nature as confirmed by differential scanning calorimetry and Fourier transform infrared and also showed enhanced release rate than the pure drug. Furthermore, a combination of IBU: PVP-K30:Tween 80 (T80) (1:2:2 w/w) homogenized nanosuspensions exhibited much smaller particle size (127 ± 6.18 nm) and two-fold faster release compared to the marketed products (DP 15 min = 95%). Other polymer combinations either did not show any significant change in particle size or exhibited agglomeration and crystal growth. Conclusion: IBU/ PVP-K30/T80 nanosuspensions were successfully prepared by high-pressure homogenization technique, with enhanced solubility and dissolution properties which could reduce the required dose and gastrointestinal side effects of the pure drug. This, in turn, is expected to increase the therapeutic benefits of IBU and other similar drugs belonging to Class II of Biopharmaceutics Classification System system, as well as to decrease/abolish the ulcerative effect. The proposed technique also has the potential of commercial scale-up to formulate safe products with higher bioavailability.

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Section: In Vitro Dissolution Of Ibu From Lyophilized Ibu: Pvp-k30nanmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

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“…Higher surface area in nanoparticles leads to higher Gibbs free energy, causing nanoparticles less stable than microparticles or larger particles [4]. This must be taken into consideration in development of nanosuspension for oral route since nanoparticles are susceptible to gastrointestinal electrolytes-induced destabilization.…”

Section: Effect Of Stabilizer Type On Particle Size and Size Distribumentioning

confidence: 99%

“…This must be taken into consideration in development of nanosuspension for oral route since nanoparticles are susceptible to gastrointestinal electrolytes-induced destabilization. Therefore, a suitable stabilizer at an optimum concentration is essential in order to maintain in vivo stability of nanosuspension [4,5]. Na-CMC, PVA, and PVP used in this study represented long chain macromolecular stabilizers which were adsorbed on the surface of cucumin nanocrystals and sterically stabilized the particles [4,6,7].…”

Section: Effect Of Stabilizer Type On Particle Size and Size Distribumentioning

confidence: 99%

Destabilization Mechanism of Ionic Surfactant on Curcumin Nanocrystal against Electrolyte

Rachmawati¹,

Rahma²,

Shaal³

et al. 2016

Preprint

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Abstract:We have successfully developed curcumin nanosuspension aimed for oral delivery. The main purpose is to improve bioavailability through enhancing its solubility. The nanoparticles were stabilized using various stabilizers including polyvinyl pyrrolidone (PVP), polyvinyl alcohol (PVA), sodium carboxymethylcellulose (Na-CMC), d-alpha tocopheryl polyethylene glycol 1000 succinate (TPGS), and sodium dodecyl sulfate (SDS). The average diameter of particles, microscopic appearance, and sedimentation of each preparation was observed and compared. Each stabilizer demonstrated different degree of inhibition of particle aggregation under electrolyte-containing simulated gastrointestinal (GIT) fluid. Non-ionic stabilizers (PVA, PVP, and TPGS) has shown to preserve the nanosuspension stability against electrolytes. In contrast, strong ionic surfactants such as SDS were found to be very sensitive to electrolytes. The results can provide useful information for the formulators to choose the most suitable stabilizers by considering the nature of stabilizers and physiological characteristics of target site of the drug.

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Micro‐ and Nanosizing of Poorly Soluble Drugs by Grinding Techniques

Scheler¹

2013

Drug Delivery Strategies for Poorly Water‐Soluble Drugs

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Characteristics of polymers enabling nano-comminution of water-insoluble drugs

Cited by 127 publications

References 26 publications

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Destabilization Mechanism of Ionic Surfactant on Curcumin Nanocrystal against Electrolyte

Micro‐ and Nanosizing of Poorly Soluble Drugs by Grinding Techniques

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